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Assay Detail

CHEMBL1246860

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Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-2 adrenergic receptor (CHEMBL210)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhalation by design: novel ultra-long-acting β(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup.
Glossop PA, Lane CA, Price DA, Bunnage ME, Lewthwaite RA, James K, Brown AD, Yeadon M, Perros-Huguet C, Trevethick MA, Clarke NP, Webster R, Jones RM, Burrows JL, Feeder N, Taylor SC, Spence FJ.
J Med Chem (2010) 53 : 6640 -6652
PubMed 20804199 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 10.18 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1242943 1 10.70
CHEMBL1243189 1 10.64
CHEMBL230490 1 10.62
CHEMBL1243158 1 10.57
CHEMBL1243348 1 10.49
CHEMBL1243190 1 10.40
CHEMBL1243256 1 10.40
CHEMBL1243222 1 10.38
CHEMBL1243101 1 10.35
CHEMBL1243285 1 10.32
CHEMBL1243407 ZINTEROL 2.0 1 10.27
CHEMBL1243317 1 10.25
CHEMBL402501 1 10.19
CHEMBL1243347 1 10.18
CHEMBL1263 SALMETEROL 4.0 1 10.15
CHEMBL1243068 1 10.04
CHEMBL1243035 1 9.89
CHEMBL1243000 1 9.77
CHEMBL1240965 1 9.68
CHEMBL1240966 1 9.62
CHEMBL1240967 PF-00610355 2.0 1 9.59
CHEMBL1242969 1 9.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1242943 EC50 = 0.02 nM 10.70
CHEMBL1243189 EC50 = 0.023 nM 10.64
CHEMBL230490 EC50 = 0.024 nM 10.62
CHEMBL1243158 EC50 = 0.027 nM 10.57
CHEMBL1243348 EC50 = 0.032 nM 10.49
CHEMBL1243190 EC50 = 0.04 nM 10.40
CHEMBL1243256 EC50 = 0.04 nM 10.40
CHEMBL1243222 EC50 = 0.042 nM 10.38
CHEMBL1243101 EC50 = 0.045 nM 10.35
CHEMBL1243285 EC50 = 0.048 nM 10.32
CHEMBL1243407 ZINTEROL EC50 = 0.054 nM 10.27
CHEMBL1243317 EC50 = 0.056 nM 10.25
CHEMBL402501 EC50 = 0.064 nM 10.19
CHEMBL1243347 EC50 = 0.066 nM 10.18
CHEMBL1263 SALMETEROL EC50 = 0.07 nM 10.15
CHEMBL1243068 EC50 = 0.091 nM 10.04
CHEMBL1243035 EC50 = 0.13 nM 9.89
CHEMBL1243000 EC50 = 0.17 nM 9.77
CHEMBL1240965 EC50 = 0.21 nM 9.68
CHEMBL1240966 EC50 = 0.24 nM 9.62
CHEMBL1240967 PF-00610355 EC50 = 0.26 nM 9.59
CHEMBL1242969 EC50 = 0.37 nM 9.43